Overview of protease inhibitors.
OBJECTIVE
To provide a basic review of the four currently available protease inhibitors: saquinavir, ritonavir, indinavir, and nelfinavir. Included are sections on surrogate markers of HIV disease and resistance to protease inhibitor therapy, as well as dosing information, pharmacokinetics, studies, adverse effects, and drug interaction potential.


METHODS
Conducted a review of published literature (MEDLINE), abstracts from national meetings and conferences, and product labeling and information available at the time of preparation through July 1997.


METHODS
Material was selected for inclusion based on relevance to objectives, publication in English, and presence of useful information for practicing pharmacists.


RESULTS
Limited published information is currently available on the protease inhibitors, especially with regard to randomized, controlled, comparative trials and establishment of guidelines for direct therapy. Much of the available information relies heavily on product information and trials that are published only in abstract form. The evaluation of the protease inhibitors (with regard to place in therapy as well as resistance and toxicities) is an ongoing process.


CONCLUSIONS
Protease inhibitors have changed opinions about the futility of the treatment of HIV disease. Protease inhibitors dramatically improve patients' surrogate markers and even show mortality benefits, especially when combined with additional antiretroviral agents. The optimism surrounding these new drugs is tempered by the toxicity profile, development of resistance, drug interaction profiles, and added costs to current regimens. Designing tolerable, effective regimens will require careful monitoring for compliance, adverse effects, and potential drug interactions.
Pakyz
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School of Pharmacy, Virginia Commonwealth University, Richmond 23298-0533, USA. Apakyz@gems.vcu.edu
Israel
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D015415:Biomarkers; D002986:Clinical Trials as Topic; D004347:Drug Interactions; D004352:Drug Resistance, Microbial; D004359:Drug Therapy, Combination; D015658:HIV Infections / Q000188:drug therapy*; D017320:HIV Protease Inhibitors / Q000008:administration & dosage / Q000009:adverse effects / Q000627:therapeutic use*; D006801:Humans
D015415:Biomarkers; D017320:HIV Protease Inhibitors